Uprima

Impotence is the inability to achieve or maintain an erection necessary for sexual intercourse. A new drug, Uprima, was developed to combat male impotence. The main active ingredient of the tablets is apomorphine hydrochloride. The auxiliary components of the drug are magnesium stearate, microcrystalline cellulose, citric acid, hypromellose, ascorbic acid, disodium edetate, silicon dioxide, iron oxide red (E172), acesulfame potassium, mint-orange flavoring agent, mannitol.

Indications Uprima

The main indications for the use of Uprim are to increase the activity of the dopaminergic neurotransmitter system of the brain in order to activate sexual interest and intensify sensations in erectile dysfunction.

Release form

Uprim is available in the form of sublingual lozenges of 2 mg (pentagonal lozenges) or 3 mg (triangular lozenges), which corresponds to the quantitative content of apomorphine hydrochloride. The red-brown tablets have double-sided engraving - the letter "a" on one side and the number 2 or 3 on the other.

Pharmacodynamics

The pharmacological action of Uprim is directed at the hypothalamus nuclei. This area of the brain is responsible for the production of dopamine, which belongs to the group of neurotransmitters and affects the ability to receive pleasure. In turn, the paraventricular nucleus of the hypothalamus is the area where aspects of sexual arousal are concentrated.

The pharmacodynamics of Uprim are determined by the properties of apomorphine, which acts as the main initiator of erection and sends pro-erectile stimuli. Restoration of erectile function becomes possible due to the normalization of the central nervous system, which affects the vascular reactions of the cavernous tissues of the penis.

Pharmacokinetics

The half-life of apomorphine is approximately 3 hours. Oral, intravenous and subcutaneous administration of the drug gives a maximum effect of 2%.

Pharmacokinetics of Uprim:

• absorption – occurs through the oral mucosa, and after 10 minutes apomorphine appears in the blood plasma (the maximum concentration is observed after 40-60 minutes);
• distribution – apomorphine is 90% bound to plasma protein (albumin);
• metabolic breakdown - occurs primarily by conjugation with glucuronic acid or sulfate. The second degradation pathway is through N-demethylation and the creation of norapomorphine, which is converted into glucuronide and sulfate conjugates;
• Uprim elimination process - sublingual administration of 2 mg of the substance causes the presence of active compounds of apomorphine approximately 90% in urine and 15% in feces. Less than 2% of apomorphine is detected in urine unchanged. Feces contain apomorphine, norapomorphine and their sulfates.

It should be noted that the pharmacokinetics of Uprim have not been studied in women or individuals under 18 years of age. Data on the pharmacokinetics of apomorphine concern healthy men over 65 years of age.

Dosing and administration

The initial dosage of Uprim is prescribed to all patients at 2 mg. The amount of tablet substance is brought to a value sufficient for sexual intercourse. The value is selected individually, and repeated administration is carried out at an 8-hour interval.

Method of administration and dosage:

• Drink some water immediately before sublingual use to help the medicine dissolve better;
• approximately 20 minutes before sexual intercourse, place the tablet under your tongue;
• the drug usually dissolves completely after 10 minutes. If the tablet has not completely dissolved after 20 minutes, the remainder should be swallowed;
• the effectiveness of the drug is increased by sexual stimulation;
• Intercourse should only begin when you feel ready for it.

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Use Uprima during pregnancy

The use of Uprim during pregnancy, by women and children is excluded.

Contraindications

Contraindications to the use of Uprim apply to patients with severe angina, a history of myocardial infarction, heart failure or hypotension, as well as diseases that limit sexual activity.

The presence of individual intolerance to one of the components of the drug will also prohibit its use.

For individuals with varying degrees of liver failure, the recommended dosage is no more than 2 mg, subject to strict medical supervision.

Particular caution should be exercised by persons with impaired renal function and anatomical changes in the penis (curvature, cavernous fibrosis, Peyronie's disease, etc.).

Since Uprima can cause dizziness or loss of consciousness, driving machines and mechanisms is allowed no earlier than 2 hours after taking the medicine.

Side effects Uprima

Data from medical observations of a group of 4,000 patients of various ages diagnosed with erectile dysfunction of organic, psigonetic or mixed origin, who took 2-3 ml of apomorphine, made it possible to identify the side effects of Uprim:

• the ability to develop a vegetative syndrome, manifested by a spontaneous and short-term drop in blood pressure, followed by loss of consciousness (if the dosage is observed, the number of cases does not exceed 0.2%);
• deterioration of the general condition, characterized by pain syndrome of various localizations or headaches;
• decreased body defenses and susceptibility to infections;
• vasodilation (blood flow due to relaxation of the muscles of the vessel walls and an increase in their lumen);
• attacks of nausea;
• drowsiness, loss of consciousness;
• feeling of shortness of breath, worsening of rhinitis/pharyngitis and increased cough;
• excessive sweating;
• changes in taste.

Taking Uprim according to a regimen agreed upon with a specialist shows good tolerability of the drug, and recorded cases of side effects are short-lived and mild.

The drug was tested on patients with liver and kidney failure, diabetes, hypertension, spinal injuries and those who had undergone prostatectomy. Side effects in the listed diseases did not differ in frequency and intensity from other patients.

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Overdose

During clinical trials, no overdose of Uprima was detected. Exceeding the dosage of the drug when administered sublingually often causes a gag reflex. Oral use of the drug significantly reduces the effect of apomorphine as a result of metabolic breakdown.

Based on the fact that there is no specific antidote for apomorphine, in case of overdose, symptomatic and general strengthening therapy is prescribed.

The drug should be taken under the control of the main vital signs - blood pressure and heart rate. It is recommended to implement methods for preventing possible orthostatic hypotension.

If you experience severe nausea, pale skin, heavy blood flow or excessive sweating, you should lie on your back and raise your legs. You should remain in this position until the negative symptoms disappear completely.

Interactions with other drugs

The conducted analysis of interaction of Uprim with other drugs (antihypertensive agents) warns against simultaneous administration of apomorphine and nitrates. Parallel use of drugs with excess dosage of Uprim (more than 5 mg) leads to occurrence of vasovagal symptoms and significant decrease in pressure during orthostasis.

A pharmacodynamic interaction between apomorphine in lozenges and centrally acting dopamine receptor agonists/antagonists has been observed.

Alcohol consumption while taking apomorphine tablets increases the frequency and severity of hypotension. At the same time, alcohol-containing drinks lead to a decrease in sexual arousal.

The drug should be administered with caution to elderly men, especially those with a history of uncontrolled hypertension, hypotension or postural hypotension, and those taking antihypertensive drugs.

It is not recommended to dissolve apomorphine tablets while taking another drug for impotence.

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Storage conditions

Storage conditions: Uprima in a place protected from direct sunlight and out of reach of children, maintaining a temperature regime of up to 25º C.

Shelf life

The shelf life of Uprim in unopened packaging is 2 years from the date of manufacture.